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TH287 hydrochloride

Catalog No. T2069L CAS 1638211-05-8

TH287 is a selective MTH1 inhibitor(IC50 : 0.8 nM). It causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.

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TH287 hydrochloride, CAS 1638211-05-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 46.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 92.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 251.00
50 mg	In stock	$ 375.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.5%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TH287 is a selective MTH1 inhibitor(IC50 : 0.8 nM). It causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
Targets&IC50	MTH1:0.8 nM
In vitro	TH287 as first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 protein in cells.?Protein co-crystal structures demonstrate that the inhibitors bind in the active site of MTH1.?The inhibitors cause incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts[1].

Molecular Weight	305.59
Formula	C11H11Cl3N4
CAS No.	1638211-05-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (89.99 mM)

References and Literature

1. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21. 2. Saleh A, et, al. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma. J Pharm Biomed Anal. 2015 Feb;104:1-11.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library DNA Damage & Repair Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TH287 hydrochloride 1638211-05-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis MTH1 inhibit Inhibitor TH287 TH287 Hydrochloride TH-287 Hydrochloride TH-287 hydrochloride TH 287 TH-287 TH 287 Hydrochloride inhibitor

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